Description
This work presents a comprehensive contemporary framework for approaching target validation in drug discovery. It begins with a detailed description of new enabling technologies, including aptamers, RNA interference, functional genomics, and proteomics. The next section looks at biologic drug development with in-depth discussion of lessons learned from such well-known cases as Erbitux, Herceptin, and Avastin. Additional targets known as "second generation" drugs, which can be identified when disease pathways are validated by biologics, present new possible small molecule therapeutics and serve as the focus of the final section of the book.
Table of Contents
I: Pharmaceutical biotechnology for target validationChapter 1: GENERATION OF TRANSGENIC ANIMALSChapter 2: TARGET VALIDATION IN CHEMOGENOMICSII: Target validation for biopharmaceutical drug discoveryChapter 3: CETUXIMAB (ERBITUX®), AN ANTI-EPIDERMAL GROWTH FACTOR RECEPTOR ANTIBODY FOR THE TREATMENT OF METASTATIC COLORECTAL CANCERChapter 4: MONOCLONAL ANTIBODY TO HER-2 IN BREAST CANCERChapter 5: VALIDATION OF TNF AS A DRUG TARGET IN INFLAMMATORY BOWEL DISEASEChapter 6: ANTI-CCL-2/MCP-1: DIRECTED BIOLOGICALS FOR INFLAMMATORY AND MALIGNANT DISEASESChapter 7: TARGETING IL-12P40 FOR IMMUNE-MEDIATED DISEASEChapter 8: THE GPIIB/IIIA ANTAGONIST ABCIXIMAB FOR ACUTE PERCUTANEOUS CORONARY INTERVENTIONIII: Validating targets of small molecule approachesChapter 9: EPIDERMAL GROWTH FACTOR RECEPTOR (EGFR) INHIBITOR FOR ONCOLOGY: DISCOVERY AND DEVELOPMENT OF ERLOTINIBChapter 10: PROGRESS IN ACHIEVING PROOF OF CONCEPT FOR p38 KINASE INHIBITORSChapter 11: IKK-2/NF-κB-DEPENDENT TRANSCRIPTIONChapter 12: TNF SIGNALING PATHWAY INHIBITORS FOR INFLAMMATION-CCR2 ANTAGONISTSChapter 13: THE DISCOVERY OF ELTROMBOPAG, AN ORALLY BIOAVAILABLE TpoR AGONISTChapter 14: ORALLY BIOAVAILABLE GLYCOPROTEIN IIB/IIIA ANTAGONISTS: A NEGATIVE CASE STUDYINDEX



